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ALSTERPAULLONE

Alsterpaullone 是高效的 CDK 抑制剂，是一种 ATP 竞争性的 GSK-3alpha/GSK-3beta 抑制剂，且作用的 IC50值都为 4 nM。它有用于神经退行性和增生性疾病的研究潜力，具有抗肿瘤活性，诱导白血病细胞凋亡。

CAS号

237430-03-4

分子式

C16H11N3O3

主要靶点

GSK-3|Apoptosis|CDK

仅限科研使用

Cat No : CM03365

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Synonyms

验证数据展示

  • CAS No.: 237430-03-4

    ALSTERPAULLONE
    CAS#: 237430-03-4

产品信息

Alsterpaullone is a Cyclin-Dependent Kinase Inhibitor, Mediated Toxicity in HeLa Cells Through Apoptosis-Inducing Effec

CAS号 237430-03-4
分子式 C16H11N3O3
主要靶点 GSK-3|Apoptosis|CDK
主要通路 凋亡|PI3K/Akt/mTOR信号通路|干细胞|细胞周期
分子量 293.28
纯度 99.39%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

Cdk1/cyclin B:35 nM|K2/Cyc E:200 nM|CDK5/p35:40 nM|cdk2/cyclin A:15 nMCD

体外活性

Alsterpaullone inhibited HeLa cells in a time-dependent (0-72 h) and dose-dependent (0-30 μ M) manner.?In the presence of alsterpaullone, HeLa cells were arrested in G2/M prior to undergoing apoptosis via a mechanism that is involved in the regulation of various antiapoptotic genes, DNA-repair, transcription, and cell cycle progression.?Compared to controls, alsterpaullone effectively prevented HeLa cells from entering S-phase.?These potential therapeutic efficacies could be correlated with the activation of caspase-3[1].

溶解度

DMSO:12 mg/mL (40.92 mM)

参考文献

1.Cui C , Wang Y , Wang Y , et al. Alsterpaullone, a Cyclin-Dependent Kinase Inhibitor, Mediated Toxicity in HeLa Cells through Apoptosis-Inducing Effect[J]. Journal of Analytical Methods in Chemistry, 2013, 2013:1-5. 2.Faria C C , Agnihotri S , Mack S C , et al. Identification of alsterpaullone as a novel small molecule inhibitor to target group 3 medulloblastoma[J]. Oncotarget, 2015, 6(25):21718-21729.

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